Molecular Classification
Enzyme, Cytochrome P450 monooxygenase
Other Names
Cytochrome P450 11B2, Steroid 11-Beta-Hydroxylase, Corticosterone Methyloxidase II, P450c11AS
Disease Roles
Aldosterone Synthase Overview
Aldosterone synthase (CYP11B2) is a mitochondrial enzyme that catalyzes the final steps in aldosterone biosynthesis. It is primarily expressed in the zona glomerulosa of the adrenal cortex and is essential for regulating electrolyte balance and blood pressure. Mutations or dysregulation in CYP11B2 can lead to hypo- or hyperaldosteronism, making it a therapeutic target for hypertension and related cardiovascular diseases. Drug development targeting CYP11B2 faces challenges due to its structural similarity to CYP11B1, necessitating highly selective inhibitors.
Mechanism of Action
Spironolactone and canrenone are mineralocorticoid receptor antagonists; direct CYP11B2 inhibitors are in development.
Biological Functions
Steroid biosynthesis
Aldosterone synthesis
Electrolyte balance regulation
Blood pressure regulation
Disease Associations
Hypertension
Hypoaldosteronism
Hyperaldosteronism
Electrolyte imbalance
Cardiovascular disease
Safety Considerations
- High sequence similarity with CYP11B1 poses a challenge for selective inhibitor design, potentially leading to off-target effects on cortisol synthesis.
- Inhibition of CYP11B2 can lead to hypoaldosteronism if not carefully monitored.
Interacting Drugs
Spironolactone
Canrenone